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1. 发明申请

US20180066013A1 Use of Excess Carbodiimide for Peptide Synthesis at Elevated Temperatures 审中-公开
公开(公告)号：US20180066013A1
公开(公告)日：2018-03-08
申请号：US15686719
申请日：2017-08-25
申请人： CEM Corporation
发明人： Jonathan M. Collins , Sandeep K. Singh
IPC分类号： C07K1/107 , C07K1/08 , C07K1/06 , C07K1/04 , C07C267/00
CPC分类号： C07K1/1075 , C07C267/00 , C07K1/04 , C07K1/045 , C07K1/061 , C07K1/082 , C07K1/084 , C07K1/10
摘要： An improved method of coupling amino acids into peptides or peptidomimetics is disclosed in which the activation and coupling are carried out in the same vessel, in the presence of a carbodiimide in an amount greater than 1 equivalent as compared to the amino acid, in the presence of an activator additive, and at a temperature greater than 30° C.

2. 发明申请

US20170342104A1 COUPLING METHOD FOR PEPTIDE SYNTHESIS AT ELEVATED TEMPERATURES 有权
公开(公告)号：US20170342104A1
公开(公告)日：2017-11-30
申请号：US15647909
申请日：2017-07-12
申请人： CEM CORPORATION
发明人： JONATHAN M. COLLINS , SANDEEP KUMAR SINGH
IPC分类号： C07K1/00 , C07K1/04 , C07K1/08 , C07K14/575
CPC分类号： C07K1/006 , C07K1/04 , C07K1/045 , C07K1/08 , C07K1/084 , C07K1/10 , C07K14/57581
摘要： An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.

3. 发明申请

US20170260247A1 Method For Synthesizing Degarelix 审中-公开
公开(公告)号：US20170260247A1
公开(公告)日：2017-09-14
申请号：US15261085
申请日：2016-09-09
申请人： Chengdu Shengnuo Biopharm Co., Ltd.
发明人： Dewen Guo , Dezhi Zeng , Guangbin Tong , Yongjun Wen
IPC分类号： C07K14/59 , C07K1/04 , C07K1/12 , C07K1/14 , C07K1/08 , C07K1/107 , C07K1/06
CPC分类号： C07K14/592 , C07K1/042 , C07K1/063 , C07K1/084 , C07K1/1077 , C07K1/122 , C07K1/14 , C07K7/06 , C07K14/59 , Y02P20/55
摘要： The present invention relates to the field of medicinal synthesis, and discloses a method for synthesizing degarelix. The method of the present invention as a whole divides the synthesis of degarelix into two parts from amino acids at positions 5 and 6, employs proper protective groups in part of the protected amino acids therein, and finally uses in association with a specific acidolysis agent to complete the whole synthesis process. In the present invention, a proper synthesizing scheme is selected, and adaptive protective group and acidolysis agent are selected, so that the overall synthesis process is optimized, the purity of degarelix is significantly improved with a higer total yield, and the production of the toxic hydantoin degradation product is avoided.

4. 发明申请

US20170204134A1 Cyclising Peptides 审中-公开
公开(公告)号：US20170204134A1
公开(公告)日：2017-07-20
申请号：US15312562
申请日：2015-05-28
申请人： The University of Durham
发明人： Steven Cobb , Christopher Coxon , Graham Sandford
IPC分类号： C07K1/08 , C07K7/52
CPC分类号： C07K1/088 , C07K1/084 , C07K1/1072 , C07K1/113 , C07K7/52
摘要： A method for preparing a cyclic peptide, derivative or analogue thereof is described. The method comprises contacting a peptide, derivative or analogue thereof with a fluoro-heteroaromatic compound to cyclise the peptide, derivative or analogue thereof.

5. 发明申请

US20170081359A1 SOLID PHASE PEPTIDE SYNTHESIS METHODS AND ASSOCIATED SYSTEMS 审中-公开
公开(公告)号：US20170081359A1
公开(公告)日：2017-03-23
申请号：US15267995
申请日：2016-09-16
申请人： Massachusetts Institute of Technology
发明人： Dale Arlington Thomas, III , Alexander James Mijalis , Bradley L. Pentelute , Mark David Simon , Andrea Adamo , Patrick Louis Heider , Klavs F. Jensen
IPC分类号： C07K1/08 , B01J19/24 , C07K14/61 , C07K7/06 , C07K14/62 , C07K14/47
CPC分类号： C07K1/084 , B01J19/24 , B01J2219/24 , C07K1/045 , C07K7/06 , C07K14/47 , C07K14/60 , C07K14/61 , C07K14/62
摘要： Methods and system for solid phase peptide synthesis are provided. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. New amino acid residues are added via a coupling reaction between an activated amino acid and an amino acid residue of the immobilized peptide. Amino acids may be activated using, e.g., a base and an activating agent. Certain inventive concepts, described herein, relate to methods and systems for the activation of amino acids. These systems and methods may allow for fewer side reactions and a higher yield compared to conventional activation techniques as well as the customization of the coupling reaction on a residue-by-residue basis without the need for costly and/or complex processes.

6. 发明授权

US07329727B2 Methods and compositions for controlled polypeptide synthesis 有权
标题翻译：受控多肽合成的方法和组合物
公开(公告)号：US07329727B2
公开(公告)日：2008-02-12
申请号：US10712967
申请日：2003-11-14
申请人： Timothy J. Deming
发明人： Timothy J. Deming
IPC分类号： C07K1/00
CPC分类号： C07K14/00 , C07K1/084 , C07K1/088 , C07K1/10 , C08G69/10
摘要： Methods and compositions for the generation of polypeptides having varied material properties are disclosed herein. Methods include means for initiating the polymerization of aminoacid-N-carboxyanhydride (NCA) monomer by combining the monomer with an amido-containing metallacycle, for making self assembling amphiphilic block copolypeptides and related protocols for adding oligo(ethyleneglycol) functionalized aminoacid-N-carboxyanhydrides (NCAs) to polyaminoacid chains. Additional methods include means of adding an end group to the carboxy terminus of a polyaminoacid chain by reacting an alloc-protected amino acid amide with a transition metal-donor ligand complex to forming an amido-amidate metallacycle for use in further polymerization reactions. Novel compositions for use in peptide synthesis and design including five and six membered amido-containing metallacycles and block copolypeptides are also disclosed.
摘要翻译：本文公开了用于产生具有不同材料性质的多肽的方法和组合物。方法包括通过将单体与含酰胺的金属环组合来引发氨基酸-N-羧酸酐（NCA）单体的聚合的手段，用于制备自组装两亲嵌段共聚肽和用于加入低聚（乙二醇）官能化的氨基酸-N-羧酸酐的相关方案（NCAs）转化为聚氨基酸链。另外的方法包括通过使分配保护的氨基酸酰胺与过渡金属给体配体络合物反应形成酰氨基脒化物金属环用于进一步聚合反应而将端基加入到聚氨基酸链的羧基末端的方法。还公开了用于肽合成和设计的新型组合物，包括含有五元和六元的含酰胺的金属螯合物和嵌段共聚肽。

7. 发明授权

US5750649A Process for producing amides using catalytic amounts of an N-hydroxy compound 失效
标题翻译：使用催化量的N-羟基化合物生产酰胺的方法
公开(公告)号：US5750649A
公开(公告)日：1998-05-12
申请号：US606104
申请日：1996-02-23
申请人： Markus Hohler , Peter Vogt
发明人： Markus Hohler , Peter Vogt
IPC分类号： C07B43/06 , C07C241/04 , C07C243/38 , C07D209/48 , C07D211/46 , C07D213/81 , C07D215/48 , C07D217/26 , C07D233/64 , C07D295/18 , C07D401/12 , C07K1/08 , C07K1/10 , C07K1/113 , C07K7/06
CPC分类号： C07K1/084
摘要： A process is disclosed for the manufacture of amides, including peptides, in which a carboxylic acid is reacted with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of N-hydroxy compound.
摘要翻译：公开了一种制备酰胺（包括肽）的方法，其中羧酸在碳二亚胺和催化量的N-羟基化合物的存在下与伯胺或仲胺反应。

8. 发明授权

US5580981A Azahydroxybenzotriazoles and derivatives thereof for peptide coupling reactions 失效
标题翻译：氮杂羟基苯并三唑及其衍生物用于肽偶联反应
公开(公告)号：US5580981A
公开(公告)日：1996-12-03
申请号：US127675
申请日：1993-09-28
申请人： Louis A. Carpino
发明人： Louis A. Carpino
IPC分类号： C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D498/04 , C07D513/04 , C07F9/6561 , C07K1/08 , C07K1/10 , C07D487/00
CPC分类号： C07F9/6561 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07K1/082 , C07K1/084 , C07K1/10
摘要： This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: ##STR1## and N-oxides thereof and salts thereof.
摘要翻译：本发明涉及在有效量的具有下式的化合物的存在下，分别由胺或醇与羧酸的酰化衍生物之间的反应形成酰胺或酯的方法：＆lt; IMAGE＆gt; 及其N-氧化物及其盐。

9. 发明授权

US4043992A Method for preparing acylated products 失效
标题翻译：酰化产物的制备方法
公开(公告)号：US4043992A
公开(公告)日：1977-08-23
申请号：US673149
申请日：1976-04-02
申请人： Yasuo Fujimoto , Nobuhiro Nakamizo
发明人： Yasuo Fujimoto , Nobuhiro Nakamizo
IPC分类号： C07C273/18 , C07K1/08 , C07C102/06
CPC分类号： C07C273/1836 , C07K1/084
摘要： Acylation of nitrogen containing compounds utilizing esters as acylation agents in the presence of salts of substituted pyridine compounds.
摘要翻译：在取代的吡啶化合物的盐存在下，使用酯作为酰化剂使含氮化合物酰化。

10. 发明授权

US3164614A New reagents for peptide synthesis 失效
标题翻译：用于肽合成的新试剂
公开(公告)号：US3164614A
公开(公告)日：1965-01-05
申请号：US11086161
申请日：1961-05-18
申请人： PARKE DAVIS & CO
发明人： NICOLAIDES ERNEST D , DE WALD HORACE A
IPC分类号： C07D309/12 , C07K1/06 , C07K1/08
CPC分类号： C07D309/12 , C07K1/065 , C07K1/084

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